Synthesis of conformationally constrained aryl- or heteroarylpiperazinyl derivatives of selected imides as 5-HT1A receptor ligands.

نویسندگان

  • Jerzy Kossakowski
  • Mariola Krawiecka
  • Bozena Kuran
چکیده

The preparation of a number of cyclic imide 5-HT(1A) receptor ligand derivatives has been described. Their structures were conformationally constrained by introducing rigid linkers containing unsaturated bonds or aromatic benzene rings. These compounds are expected to possess anxiolytic and antidepressant activity.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis of New 1-Aryl-4-(biarylmethylene)piperazine Ligands, Structurally Related to Adoprazine (SLV313)

A series of new 1-aryl-4-(biarylmethylene)piperazines has been synthesized. These ligands are structurally related to SLV-313, a potential atypical antipsychotic having potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling reactions of 1-boc-piperazine with appropriate aryl halides and subsequent removal of the boc group rendered arylpiperazines. The re...

متن کامل

Synthesis of a carbon-14 analogue of N-(aryl-methyl)-3-phenyl-acryl amidine-[carboxy-14C] and its derivatives as NR2B-selective NMDA receptor antagonist

Four amidine NR2B-selective NMDA receptor antagonists, N-( 2-methoxy benzyl) -3-phenyl-acrylamidine, N-[diduterio(2-methoxyphenyl) methyl]-3-phenyl-acrylamidine, N-benzyl-3-phenyl-acryl amidine and N-[diduterio(phenyl)methyl]-3-phenyl-acrylamidine, all fourlabeled with carbon-14 in the 1-position, have been synthesized as part of 5-step sequence fromBa14CO3.

متن کامل

Synthesis and docking study on thiadiazolo[3,2-a][1,3]diazepin-8(5H)-one derivatives as selective GABA(A) agonists

HIE-124 is a new member of ultra-short acting hypnotics’ drug family. In this research, the synthesis ofanalogues of HIE-124 drug in the heterocyclic thiazole ring replaced to thiadiazole, will be presented.Thiadiazolodiazepines during a two-step reaction starting from the amino thiadiazole resultedfrom-various derivatives of benzoic acid and thiosemicarbazide were synthesized. In the first ste...

متن کامل

New imide 5-HT1A receptor ligands - modification of terminal fragment geometry.

Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moieties derived from NAN190, were synthesized and evaluated in vitro for their ability to bind to the serotonin 5-HT(1A) and 5-HT(2A) receptors. All new derivatives from series a demonstrated high 5-HT(1A) affinities, whereas THIQ analogues were mu...

متن کامل

New 8-aminoalkyl derivatives of purine-2,6-dione with arylalkyl, allyl or propynyl substituents in position 7, their 5-HT1A, 5-HT2A, and 5-HT7 receptor affinity and pharmacological evaluation.

BACKGROUND Our previous studies in a group of arylpiperazine derivatives of 1,3-dimethyl-3,7-dihydro-purine-2,6-diones, aimed at chemical diversification of the purine-2,6-dione by introduction of hydrophobic substituent in a 7- or 8- position or elongation of the linker length between arylpiperazine and purine core, allowed a selection of potent 5-HT1A, 5-HT2A and 5-HT7 receptor ligands displa...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Molecules

دوره 11 8  شماره 

صفحات  -

تاریخ انتشار 2006